Bemesetron Explained

Bemesetron (MDL-72222) is a drug which acts as an antagonist at the 5HT₃ receptor.^[1] It has antiemetic effects comparable to metoclopramide,^[2] however it is not used clinically, instead its main application is in scientific research studying the involvement of the 5HT₃ receptor in the actions of drugs of abuse.^{[3] [4] [5] [6]}

See also

• Tropanserin
• Tropisetron
• Zatosetron
• Ricasetron
• Granisetron

Notes and References

1. Shearman GT, Tolcsvai L . Effect of the selective 5-HT3 receptor antagonists ICS 205-930 and MDL 72222 on 5-HTP-induced head shaking and behavioral symptoms induced by 5-methoxy-N,N,dimethyltryptamine in rats: comparison with some other 5-HT receptor antagonists . Psychopharmacology . 92 . 4 . 520–3 . 1987 . 3114804 . 10.1007/bf00176488. 25814825 .
2. Homesley HD, Hahne WF, McLees B . Randomized comparison of the antiemetic efficacy of a serotonin type 3 receptor antagonist (MDL 72,222) with a high-dose metoclopramide regimen . Am. J. Clin. Oncol. . 16 . 2 . 175–9 . April 1993 . 8452114 . 10.1097/00000421-199304000-00020. 11733418 . etal.
3. McKinzie DL, McBride WJ, Murphy JM, Lumeng L, Li TK . Effects of MDL 72222, a serotonin3 antagonist, on operant responding for ethanol by alcohol-preferring P rats . Alcohol. Clin. Exp. Res. . 24 . 10 . 1500–4 . October 2000 . 11045857 . 10.1111/j.1530-0277.2000.tb04567.x.
4. Kankaanpää A, Meririnne E, Seppälä T . 5-HT3 receptor antagonist MDL 72222 attenuates cocaine- and mazindol-, but not methylphenidate-induced neurochemical and behavioral effects in the rat . Psychopharmacology . 159 . 4 . 341–50 . February 2002 . 11823886 . 10.1007/s00213-001-0939-4. 21614467 .
5. Kos T, Popik P, Pietraszek M . Effect of 5-HT3 receptor antagonist MDL 72222 on behaviors induced by ketamine in rats and mice . Eur Neuropsychopharmacol . 16 . 4 . 297–310 . May 2006 . 16288851 . 10.1016/j.euroneuro.2005.10.001 . 43575963 . etal.
6. Yoo JH, Nam YS, Lee SY, Jang CG . Dopamine neurotransmission is involved in the attenuating effects of 5-HT3 receptor antagonist MDL 72222 on acute methamphetamine-induced locomotor hyperactivity in mice . Synapse . 62 . 1 . 8–13 . January 2008 . 17948891 . 10.1002/syn.20461. 20699645 .